TABLE 1

Biodistribution of 111In-DOTA-Nle-CycMSHhex in B16/F1 Melanoma–Bearing C57 Mice

Biodistribution at…
Tissue0.5 h2 h4 h24 h2-h NDP blockade2-h L-lysine coinjection
%ID/g*
 Tumor24.94 ± 4.5819.39 ± 1.6517.01 ± 2.5410.53 ± 1.110.81 ± 0.0314.48 ± 3.25
 Brain0.21 ± 0.070.02 ± 0.010.06 ± 0.030.03 ± 0.010.01 ± 0.010.04 ± 0.01
 Blood3.33 ± 0.350.11 ± 0.070.05 ± 0.020.02 ± 0.010.07 ± 0.050.92 ± 0.48
 Heart1.24 ± 0.150.16 ± 0.100.12 ± 0.030.07 ± 0.050.06 ± 0.020.37 ± 0.02
 Lung2.45 ± 0.830.32 ± 0.100.10 ± 0.050.10 ± 0.030.30 ± 0.060.75 ± 0.21
 Liver2.75 ± 0.261.46 ± 0.201.72 ± 0.071.89 ± 0.141.46 ± 0.081.42 ± 0.30
 Spleen1.09 ± 0.330.41 ± 0.130.47 ± 0.130.32 ± 0.080.44 ± 0.020.43 ± 0.07
 Stomach3.20 ± 0.981.25 ± 0.241.49 ± 0.121.34 ± 0.420.36 ± 0.141.64 ± 0.78
 Kidneys16.20 ± 4.329.52 ± 0.449.99 ± 1.399.31 ± 0.9111.56 ± 0.566.66 ± 0.62
 Muscle0.60 ± 0.220.15 ± 0.080.10 ± 0.080.03 ± 0.010.02 ± 0.010.10 ± 0.08
 Pancreas1.18 ± 0.380.14 ± 0.020.16 ± 0.020.23 ± 0.080.12 ± 0.020.21 ± 0.05
 Bone1.34 ± 0.400.18 ± 0.100.22 ± 0.150.16 ± 0.030.05 ± 0.040.55 ± 0.14
 Skin4.11 ± 0.720.66 ± 0.230.53 ± 0.050.64 ± 0.160.29 ± 0.021.02 ± 0.09
%ID*
 Intestines2.16 ± 0.281.40 ± 0.563.03 ± 1.061.41 ± 0.861.14 ± 0.471.85 ± 0.73
 Urine57.00 ± 3.9182.23 ± 5.8384.61 ± 5.2187.29 ± 3.6092.25 ± 1.5676.79 ± 5.35
Tumor–to–normal-tissue uptake ratio
 Tumor-to-blood7.49176.27340.20526.5011.5715.74
 Tumor-to-kidneys1.542.041.701.130.072.17
 Tumor-to-lung10.1860.59170.10105.302.7019.31
 Tumor-to-liver9.0713.289.895.570.5510.20
 Tumor-to-muscle41.57129.27170.10351.0040.50144.80
 Tumor-to-skin6.0729.3832.0916.452.7914.20
  • * Mean ± SD (n = 5).

  • P < 0.05, significance comparison between tumor uptake of 111In-DOTA-Nle-CycMSHhex with or without NDP-MSH blockade and kidney uptake of 111In-DOTA-Nle-CycMSHhex with or without L-lysine coinjection.

  • Data are presented as percent %ID/g or as %ID (mean ± SD, n = 5).